Enzyme-catalyzed activation of anticancer prodrugs

The following endogenous enzymes are discussed: aldehyde oxidase, amino acid oxidase, cytochrome P reductase, DT-diaphorase, cytochrome P, tyrosinase, thymidylate synthase, thymidine phosphorylase, glutathione S-transferase, deoxycytidine kinase, carboxylesterase, alkaline phosphatase, beta-glucuronidase and cysteine conjugate beta-lyase. In relation to each of these enzymes, several prodrugs are discussed regarding organ- or tumor-selective activation of clinically relevant prodrugs of 5-fluorouracil, axazaphosphorines cyclophosphamide, ifosfamide, and trofosfamide , paclitaxel, etoposide, anthracyclines doxorubicin, daunorubicin, epirubicin , mercaptopurine, thioguanine, cisplatin, melphalan, and other important prodrugs such as menadione, mitomycin C, tirapazamine, 5- aziridinyl -2,4-dinitrobenzamide, ganciclovir, irinotecan, dacarbazine, and amifostine.

In addition to endogenous enzymes, a number of nonendogenous enzymes, used in antibody-, gene-, and virus-directed enzyme prodrug therapies, are described. J Gene Med , 2 3 , 01 May Cited by: articles PMID: Stem Cells , 13 5 , 01 Sep Cited by: 16 articles PMID: Connors TA. Gene Ther , 2 10 , 01 Dec Cited by: 64 articles PMID: Contact us.

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A subscription may be required. Martijn Rooseboom Search articles by 'Martijn Rooseboom'. Rooseboom M ,. Commandeur JN ,. Vermeulen NP. Affiliations All authors 1. Share this article Share with email Share with twitter Share with linkedin Share with facebook. Abstract The rationale fo the development of prodrugs relies upon delivery of higher concentrations of a drug to target cells compared to administration of the drug itself. In the last decades, numerous prodrugs that are enzymatically activated into anti-cancer agents have been developed.

This review describes the most important enzymes involved in prodrug activation notably with respect to tissue distribution, up-regulation in tumor cells and turnover rates. The following endogenous enzymes are discussed: aldehyde oxidase, amino acid oxidase, cytochrome P reductase, DT-diaphorase, cytochrome P, tyrosinase, thymidylate synthase, thymidine phosphorylase, glutathione S-transferase, deoxycytidine kinase, carboxylesterase, alkaline phosphatase, beta-glucuronidase and cysteine conjugate beta-lyase.

Molecular and Computational Toxicology. Overview Fingerprint. Abstract The rationale for the development of prodrugs relies upon delivery of higher concentrations of a drug to target cells compared to administration of the drug itself.

Access to Document Fingerprint Dive into the research topics of 'Enzyme-catalyzed activation of anticancer prodrugs'. Together they form a unique fingerprint. View full fingerprint. Pharmacological Reviews , 56 1 , Rooseboom, M.